Pub Date : 2026-02-10Epub Date: 2025-12-31DOI: 10.1016/j.ijpharm.2025.126552
Kaixin Feng , Zhongkun Zhang , Jingjing Zhang , Xiaohan Xia , Siyu Yao , Yufei Wang , Min Wu
Doxorubicin (DOX) is limited by its clinical toxicity as a breast cancer therapy. Traditional liposomal formulations improve the tumor delivery of DOX but suffer from inadequate controlled release and low encapsulation efficiency of DOX. To address these, we developed a photo-responsive liposomal formulation DTTPL by co-encapsulating DOX and TiO2 nanostructures (TiO2) within D-α-tocopheryl succinate (α-TOS)-PEG liposomes. DTTPL successfully facilitated the release of DOX through the light-sensitive catalysis mechanism of TiO2, exhibiting 4.6 times greater cytotoxicity against MCF-7 cells compared to free DOX. Transcriptional analysis revealed synergistic DOX/DTTPL dysregulation of key genes (Brca1, Bcl-2, Bax, Caspase-3), aligning with cytotoxicity. Eventually, light-triggered DOX/DTTPL formulation resulted in 70.09% of tumor growth inhibition (TGI) in mice with no significant organ toxicity. This photo-responsive nanoformulation enables efficient controlled release of DOX, offering an alternative strategy for small molecule delivery to treat triple negative breast cancer.
{"title":"Light-responsive α-TOS liposomal nanocarriers Co-delivering TiO2 and doxorubicin for the treatment of breast cancer","authors":"Kaixin Feng , Zhongkun Zhang , Jingjing Zhang , Xiaohan Xia , Siyu Yao , Yufei Wang , Min Wu","doi":"10.1016/j.ijpharm.2025.126552","DOIUrl":"10.1016/j.ijpharm.2025.126552","url":null,"abstract":"<div><div>Doxorubicin (DOX) is limited by its clinical toxicity as a breast cancer therapy. Traditional liposomal formulations improve the tumor delivery of DOX but suffer from inadequate controlled release and low encapsulation efficiency of DOX. To address these, we developed a photo-responsive liposomal formulation DTTPL by co-encapsulating DOX and TiO<sub>2</sub> nanostructures (TiO<sub>2</sub>) within D-α-tocopheryl succinate (α-TOS)-PEG liposomes. DTTPL successfully facilitated the release of DOX through the light-sensitive catalysis mechanism of TiO<sub>2</sub>, exhibiting 4.6 times greater cytotoxicity against MCF-7 cells compared to free DOX. Transcriptional analysis revealed synergistic DOX/DTTPL dysregulation of key genes (Brca1, Bcl-2, Bax, Caspase-3), aligning with cytotoxicity.<!--> <!-->Eventually, light-triggered DOX/DTTPL formulation resulted in 70.09% of tumor growth inhibition (TGI) in mice with no significant organ toxicity. This photo-responsive nanoformulation enables efficient controlled release of DOX, offering an alternative strategy for small molecule delivery to treat triple negative breast cancer.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"690 ","pages":"Article 126552"},"PeriodicalIF":5.2,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145892405","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-02-10Epub Date: 2025-12-28DOI: 10.1016/j.ijpharm.2025.126529
Shelly Keisar , Qonita Kurnia Anjani , Abraham M. Abraham , Lalitkumar K. Vora , Eneko Larrañeta , Ryan F. Donnelly , Aiman Abu Ammar
Microneedles (MNs) are micro-sized needles that were originally designed as minimally invasive and painless devices capable of piercing the main skin barrier, the stratum corneum, without stimulating nerve fibers, showing promising prospects as an alternative to other drug administration routes. Poly (lactic-co-glycolic acid) (PLGA) is a biodegradable and biocompatible copolymer with favorable mechanical properties, making it particularly suitable for fabrication of MNs for controlled-release drug delivery. This review provides a comprehensive overview of the design, fabrication, and therapeutic potential of PLGA-based MN systems across a broad range of applications, including transdermal systemic delivery, vaccine delivery and topical skin applications. Due to their exceptional virtues, PLGA MNs are further utilized in nontransdermal applications such as ocular, oral cavity, nasal, and other emerging uses that are presented. Eventually, toxicity and safety profile are discussed, and a concluding section on future perspectives is provided.
{"title":"Poly (lactic-co-glycolic acid)-based microneedles for drug delivery across different biological barriers","authors":"Shelly Keisar , Qonita Kurnia Anjani , Abraham M. Abraham , Lalitkumar K. Vora , Eneko Larrañeta , Ryan F. Donnelly , Aiman Abu Ammar","doi":"10.1016/j.ijpharm.2025.126529","DOIUrl":"10.1016/j.ijpharm.2025.126529","url":null,"abstract":"<div><div>Microneedles (MNs) are micro-sized needles that were originally designed as minimally invasive and painless devices capable of piercing the main skin barrier, the <em>stratum corneum</em>, without stimulating nerve fibers, showing promising prospects as an alternative to other drug administration routes. Poly (lactic-co-glycolic acid) (PLGA) is a biodegradable and biocompatible copolymer with favorable mechanical properties, making it particularly suitable for fabrication of MNs for controlled-release drug delivery. This review provides a comprehensive overview of the design, fabrication, and therapeutic potential of PLGA-based MN systems across a broad range of applications, including transdermal systemic delivery, vaccine delivery and topical skin applications. Due to their exceptional virtues, PLGA MNs are further utilized in nontransdermal applications such as ocular, oral cavity, nasal, and other emerging uses that are presented. Eventually, toxicity and safety profile are discussed, and a concluding section on future perspectives is provided.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"690 ","pages":"Article 126529"},"PeriodicalIF":5.2,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145862473","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-02-10Epub Date: 2025-12-26DOI: 10.1016/j.ijpharm.2025.126524
Siqi Wang, Rand Z. Murtadha, R. Karl Malcolm
There have been several significant advances in recent years around long-acting strategies for HIV pre-exposure prophylaxis, including DapiRing® (a 1-month dapivirine (DPV)-releasing vaginal ring), Apretude® (a cabotegravir intramuscular injection administered every two months), and Yeztugo® (a twice-yearly lenacapavir injection). With the goal of developing new drug delivery devices that can extend antiretroviral release for 12 months or longer, we report here our preliminary efforts to design a subdermal implant releasing the antiretroviral drug DPV. These reservoir-type rod implants (length 40 mm, cross-sectional diameters 2.5, 3.2, 3.5 or 4.0 mm) comprised a silicone elastomer core containing solid crystalline DPV (loading 10, 20 or 40 % w/w) and an open-ended non-medicated rate-controlling silicone elastomer membrane (thickness 0.5, 0.8 or 1.0 mm). DPV in vitro release rates could be modulated by adjusting the membrane thickness. Continuous in vitro DPV release ∼12 μg/day was demonstrated over 330 days, with sufficient residual drug content (∼87 mg/∼95 %) to extend release for at least 5 years. In particular, the study highlights the challenges in designing subdermal implants providing sufficient DPV release to maintain systemic/vaginal concentrations at protective levels.
{"title":"Formulation development of a dapivirine-releasing subdermal implant for HIV prevention","authors":"Siqi Wang, Rand Z. Murtadha, R. Karl Malcolm","doi":"10.1016/j.ijpharm.2025.126524","DOIUrl":"10.1016/j.ijpharm.2025.126524","url":null,"abstract":"<div><div>There have been several significant advances in recent years around long-acting strategies for HIV pre-exposure prophylaxis, including DapiRing® (a 1-month dapivirine (DPV)-releasing vaginal ring), Apretude® (a cabotegravir intramuscular injection administered every two months), and Yeztugo® (a twice-yearly lenacapavir injection). With the goal of developing new drug delivery devices that can extend antiretroviral release for 12 months or longer, we report here our preliminary efforts to design a subdermal implant releasing the antiretroviral drug DPV. These reservoir-type rod implants (length 40 mm, cross-sectional diameters 2.5, 3.2, 3.5 or 4.0 mm) comprised a silicone elastomer core containing solid crystalline DPV (loading 10, 20 or 40 % w/w) and an open-ended non-medicated rate-controlling silicone elastomer membrane (thickness 0.5, 0.8 or 1.0 mm). DPV <em>in vitro</em> release rates could be modulated by adjusting the membrane thickness. Continuous <em>in vitro</em> DPV release ∼12 μg/day was demonstrated over 330 days, with sufficient residual drug content (∼87 mg/∼95 %) to extend release for at least 5 years. In particular, the study highlights the challenges in designing subdermal implants providing sufficient DPV release to maintain systemic/vaginal concentrations at protective levels.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"690 ","pages":"Article 126524"},"PeriodicalIF":5.2,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145849913","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The objective of this study was to develop vitamin E nanobarrier contact lenses that can sustain the delivery of an equivalent amount of cysteamine to the cornea as eight drops per day regimen used in treating cystinosis. Senofilcon A lenses (14.0 mm diameter, −0.50 D power, 8.4 mm base curve) integrated with vitamin E and cysteamine were tested for drug release and fitted to the sink-release model to determine diffusivity and partition coefficient. The pharmacokinetics of cysteamine delivery by contact lenses and by control eye drops was measured in New Zealand white rabbits. Cysteamine delivery was modeled by a mechanistic model using contact lens parameters obtained from the in vitro studies along with known anatomical, physiological and drug specific parameters obtained from literature. The release duration of cysteamine increased from a few minutes in control lenses to about 2 and 6 h, in lenses loaded with 20 and 30 % vitamin E, respectively. In vivo studies showed that the contact lens-based approach can deliver significantly high concentrations compared to eye drops. The total mass of drug delivered by 20 % vitamin E loaded contact lens is more than six times the mass delivered by a single eye drop. The contact lens-based therapy achieves higher delivery than drops in the back of the eye tissues as well. The predictions of the mechanistic mathematical model are in good agreement with in vivo measurements for both eye drops and contact lenses. The contact lens-based delivery of cysteamine is a promising approach for replacing the multiple drop therapy.
{"title":"Cysteamine-eluting contact lenses: integrating in vitro, in vivo, and in silico approaches for ocular drug delivery","authors":"Anuj Chauhan , Sarbani Hazra , Brock Matter , Pankaj Kumar Sharma , Shilpa George , Aishee Dey , Bommanahalli Nagaraju Kumara , Uday B. Kompella","doi":"10.1016/j.ijpharm.2025.126528","DOIUrl":"10.1016/j.ijpharm.2025.126528","url":null,"abstract":"<div><div>The objective of this study was to develop vitamin E nanobarrier contact lenses that can sustain the delivery of an equivalent amount of cysteamine to the cornea as eight drops per day regimen used in treating cystinosis. Senofilcon A lenses (14.0 mm diameter, −0.50 D power, 8.4 mm base curve) integrated with vitamin E and cysteamine were tested for drug release and fitted to the sink-release model to determine diffusivity and partition coefficient. The pharmacokinetics of cysteamine delivery by contact lenses and by control eye drops was measured in New Zealand white rabbits. Cysteamine delivery was modeled by a mechanistic model using contact lens parameters obtained from the in vitro studies along with known anatomical, physiological and drug specific parameters obtained from literature. The release duration of cysteamine increased from a few minutes in control lenses to about 2 and 6 h, in lenses loaded with 20 and 30 % vitamin E, respectively. In vivo studies showed that the contact lens-based approach can deliver significantly high concentrations compared to eye drops. The total mass of drug delivered by 20 % vitamin E loaded contact lens is more than six times the mass delivered by a single eye drop. The contact lens-based therapy achieves higher delivery than drops in the back of the eye tissues as well. The predictions of the mechanistic mathematical model are in good agreement with in vivo measurements for both eye drops and contact lenses. The contact lens-based delivery of cysteamine is a promising approach for replacing the multiple drop therapy.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"690 ","pages":"Article 126528"},"PeriodicalIF":5.2,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145827581","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-02-10Epub Date: 2026-01-02DOI: 10.1016/j.ijpharm.2026.126554
Ilaria Polidori , Leonie Iris Weber , Stefan Keim , Dennis To , Markus Hartl , Andreas Bernkop-Schnürch
Enzyme-responsive lipid nanoparticles (LNPs) offer a promising strategy for oral nucleic acid delivery to gastrointestinal tumors. We hypothesized that coating LNPs with polyphosphates (PP) would enhance mucus penetration and enable charge conversion upon activation by intestinal alkaline phosphatase (IAP). The presence of the cell-penetrating peptide (CPP) stearyl-D-Arg8 provides enhanced cellular uptake. LNPs were characterized regarding size, polydispersity index, zeta potential, charge conversion and evaluated for pH stability, behaviour in biorelevant fluids, and mucus diffusion. Plasmid DNA encoding for GFP or brain acid soluble protein-1 (BASP1) was encapsulated, and uptake and transfection were studied in intestinal cancer cell lines. Upon incubation with IAP, PP-coated D-Arg8-LNPs released phosphate groups and underwent charge conversion. These particles remained stable across pH 1.5–9.0 and were more resistant to biorelevant fluids, though destabilization occurred with digestive enzymes. Compared to DOTAP- and D-Arg8-LNPs, PP-coated LNPs showed superior mucus diffusion, cellular uptake, and transfection efficiency in hard-to-transfect Caco-2 and SW480 cells. Importantly, BASP1 expression from LNPs effectively suppressed SW480 proliferation. Overall, PP coated LNPs for oral administration can efficiently deliver nucleic acids into intestinal tumor cells, which may be suitable to interfere with the tumorigenic phenotype.
{"title":"Alkaline phosphatase-triggered charge converting lipid nanoparticles: An innovative approach for oral nucleic acid delivery","authors":"Ilaria Polidori , Leonie Iris Weber , Stefan Keim , Dennis To , Markus Hartl , Andreas Bernkop-Schnürch","doi":"10.1016/j.ijpharm.2026.126554","DOIUrl":"10.1016/j.ijpharm.2026.126554","url":null,"abstract":"<div><div>Enzyme-responsive lipid nanoparticles (LNPs) offer a promising strategy for oral nucleic acid delivery to gastrointestinal tumors. We hypothesized that coating LNPs with polyphosphates (PP) would enhance mucus penetration and enable charge conversion upon activation by intestinal alkaline phosphatase (IAP). The presence of the cell-penetrating peptide (CPP) stearyl-D-Arg<sub>8</sub> provides enhanced cellular uptake. LNPs were characterized regarding size, polydispersity index, zeta potential, charge conversion and evaluated for pH stability, behaviour in biorelevant fluids, and mucus diffusion. Plasmid DNA encoding for GFP or brain acid soluble protein-1 (BASP1) was encapsulated, and uptake and transfection were studied in intestinal cancer cell lines. Upon incubation with IAP, PP-coated D-Arg<sub>8</sub>-LNPs released phosphate groups and underwent charge conversion. These particles remained stable across pH 1.5–9.0 and were more resistant to biorelevant fluids, though destabilization occurred with digestive enzymes. Compared to DOTAP- and D-Arg<sub>8</sub>-LNPs, PP-coated LNPs showed superior mucus diffusion, cellular uptake, and transfection efficiency in hard-to-transfect Caco-2 and SW480 cells. Importantly, BASP1 expression from LNPs effectively suppressed SW480 proliferation. Overall, PP coated LNPs for oral administration can efficiently deliver nucleic acids into intestinal tumor cells, which may be suitable to interfere with the tumorigenic phenotype.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"690 ","pages":"Article 126554"},"PeriodicalIF":5.2,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145900302","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-02-10Epub Date: 2025-12-28DOI: 10.1016/j.ijpharm.2025.126540
Siqi Chen, Yizhen Yan, Jiayi Zou, Xin He, Kexin Li
Multi-modal combination therapy for tumors can overcome the limitations of single-modal therapy and bring new opportunities for high-efficient tumor treatment. Nevertheless, how to ingeniously design functionalized nanocarriers to mediate the synergistict effects among various therapeutic approaches remains a core challenge. In this study, we developed a polydopamine (PDA) coated outside and glucose oxidase (GOx) adsorbed inside copper-doped zeolitic imidazolate framework-8 (CZ8) with metformin hydrochloride (MET) / doxorubicin (DOX) as a multifunctional nano-codelivery system, abbreviated as PMDGCZ8, which could focus more on the synergy and continuity of multiple therapies including photothermal therapy (PTT), chemodynamic therapy (CDT), starving tumor therapy (STT) and chemotherapy (CT). Herein, PMDGCZ8 innovatively combined the gating effect of PDA membrane with the pH sensitivity of CZ8 skeleton to form a dual-responsive bomb that could trigger release on demand and significantly improve the accuracy of tumor localization. Furthermore, we also incorporated the strategies of reshaping the tumor hypoxia and immunosuppressive microenvironment into the synergistic treatment process in order to achieve a comprehensive anti-tumor ecological network. Both in vitro and in vivo experiments suggested that PMDGCZ8 significantly enhanced drug accumulation on tumors, reduced systemic toxicity, activated anti-tumor immune response, further inhibited the recurrence and metastasis, and consequently was expected to become a new type of nano-delivery platform with great development potential.
{"title":"An intelligent responsive ZIF-8 co-delivery nanoplatform with multimodal synergistic technologies for closed-loop therapy of tumors","authors":"Siqi Chen, Yizhen Yan, Jiayi Zou, Xin He, Kexin Li","doi":"10.1016/j.ijpharm.2025.126540","DOIUrl":"10.1016/j.ijpharm.2025.126540","url":null,"abstract":"<div><div>Multi-modal combination therapy for tumors can overcome the limitations of single-modal therapy and bring new opportunities for high-efficient tumor treatment. Nevertheless, how to ingeniously design functionalized nanocarriers to mediate the synergistict effects among various therapeutic approaches remains a core challenge. In this study, we developed a polydopamine (PDA) coated outside and glucose oxidase (GOx) adsorbed inside copper-doped zeolitic imidazolate framework-8 (CZ8) with metformin hydrochloride (MET) / doxorubicin (DOX) as a multifunctional nano-codelivery system, abbreviated as PMDGCZ8, which could focus more on the synergy and continuity of multiple therapies including photothermal therapy (PTT), chemodynamic therapy (CDT), starving tumor therapy (STT) and chemotherapy (CT). Herein, PMDGCZ8 innovatively combined the gating effect of PDA membrane with the pH sensitivity of CZ8 skeleton to form a dual-responsive bomb that could trigger release on demand and significantly improve the accuracy of tumor localization. Furthermore, we also incorporated the strategies of reshaping the tumor hypoxia and immunosuppressive microenvironment into the synergistic treatment process in order to achieve a comprehensive anti-tumor ecological network. Both in vitro and <em>in vivo</em> experiments suggested that PMDGCZ8 significantly enhanced drug accumulation on tumors, reduced systemic toxicity, activated anti-tumor immune response, further inhibited the recurrence and metastasis, and consequently was expected to become a new type of nano-delivery platform with great development potential.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"690 ","pages":"Article 126540"},"PeriodicalIF":5.2,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145862390","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Near-infrared (NIR) spectroscopy is a nondestructive analytical technique that is increasingly considered for inclusion in Process Analytical Technology (PAT) frameworks and for 100% inspection, with the potential to raise pharmaceutical product quality. While reflectance-based NIR systems already deliver throughputs suitable for commercial manufacturing, transmission-based NIR systems, although offering superior predictive accuracy for active pharmaceutical ingredient (API) content in tablets, have been throughput-limited. Recently, a newly developed transmission NIR spectrometer has been shown to acquire precise tablet spectra within a few milliseconds. In this study, a spectrometer was integrated into a belt-conveyor transport apparatus to create a high-throughput analytical system for pharmaceutical tablets. A throughput of 186,000 tablets per hour was achieved, demonstrating 100% API content measurement and real-time rejection of out-of-specification tablets.
{"title":"A commercial-scale high-throughput near-infrared transmission spectroscopy system for full inspection of active pharmaceutical ingredient content in all tablets","authors":"Junki Sahara , Katsuhiko Nishiyama , Kazuki Shinoyama , Aya Ikarashi , Takuma Yokoyama , Shinya Matsuda , Kenji Yoshii , Masaya Fujimoto , Yasufumi Yagisawa , Koji Nakayama , Tomoaki Sakamoto","doi":"10.1016/j.ijpharm.2025.126516","DOIUrl":"10.1016/j.ijpharm.2025.126516","url":null,"abstract":"<div><div>Near-infrared (NIR) spectroscopy is a nondestructive analytical technique that is increasingly considered for inclusion in Process Analytical Technology (PAT) frameworks and for 100% inspection, with the potential to raise pharmaceutical product quality. While reflectance-based NIR systems already deliver throughputs suitable for commercial manufacturing, transmission-based NIR systems, although offering superior predictive accuracy for active pharmaceutical ingredient (API) content in tablets, have been throughput-limited. Recently, a newly developed transmission NIR spectrometer has been shown to acquire precise tablet spectra within a few milliseconds. In this study, a spectrometer was integrated into a belt-conveyor transport apparatus to create a high-throughput analytical system for pharmaceutical tablets. A throughput of 186,000 tablets per hour was achieved, demonstrating 100% API content measurement and real-time rejection of out-of-specification tablets.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"690 ","pages":"Article 126516"},"PeriodicalIF":5.2,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145819254","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ERAP2 is an enzyme essential in the preparation of mature antigen from peptide precursors. Inhibitors of this enzyme can find applications in immuno-oncology and in the treatment of autoimmune diseases including psoriasis and ankylosing spondylitis. In recent years, electrospinning has attracted considerable interest in the field of drug delivery. The potential applications of electrospun fibers in the treatment of skin and arthritis diseases are significant. This can be attributed to the fibers’ structural similarity to the extracellular matrix, in addition to their capacity to encapsulate disease-modifying anti-inflammatory agents. Electrospun fibrous mats are also used as drug delivery systems for loading potential anticancer drugs, with the aim of killing cancer cells. This allows for enhanced tumour penetration, increased drug retention, and higher drug delivery.
The objective of this project was to evaluate the production of meshes using electrospun poly(ε-Caprolactone) (PCL), and poly-(vinyl alcohol) (PVA) fibrous patches, loaded with an ERAP2 inhibitor, with or without liposomes. An examination was conducted to ascertain the physicochemical properties, including morphology and structure. The loading, release and stability of the inhibitor was studied by both UV–Vis and MS spectroscopy. The cytotoxic assay demonstrated the biocompatibility of the fabricated nanomats of PVA and PVA-liposome (PVA-L) formulations. In vitro assays demonstrated the compatibility of meshes with cell growth, ERAP2 engagement and antigen presentation. The results of the study validated the potential for future applications in the specified therapeutic areas.
{"title":"ERAP2 inhibitor −incorporated nanofibers: Characterization and biological assessment","authors":"Filipa Vasconcelos , Laetitia Lesire , Adrien Herledan , Catherine Piveteau , Benoit Deprez , Hermis Iatrou , Rebecca Deprez-Poulain","doi":"10.1016/j.ijpharm.2026.126555","DOIUrl":"10.1016/j.ijpharm.2026.126555","url":null,"abstract":"<div><div>ERAP2 is an enzyme essential in the preparation of mature antigen from peptide precursors. Inhibitors of this enzyme can find applications in immuno-oncology and in the treatment of autoimmune diseases including psoriasis and ankylosing spondylitis. In recent years, electrospinning has attracted considerable interest in the field of drug delivery. The potential applications of electrospun fibers in the treatment of skin and arthritis diseases are significant. This can be attributed to the fibers’ structural similarity to the extracellular matrix, in addition to their capacity to encapsulate disease-modifying anti-inflammatory agents. Electrospun fibrous mats are also used as drug delivery systems for loading potential anticancer drugs, with the aim of killing cancer cells. This allows for enhanced tumour penetration, increased drug retention, and higher drug delivery.</div><div>The objective of this project was to evaluate the production of meshes using electrospun poly(ε-Caprolactone) (PCL), and poly-(vinyl alcohol) (PVA) fibrous patches, loaded with an ERAP2 inhibitor, with or without liposomes. An examination was conducted to ascertain the physicochemical properties, including morphology and structure. The loading, release and stability of the inhibitor was studied by both UV–Vis and MS spectroscopy. The cytotoxic assay demonstrated the biocompatibility of the fabricated nanomats of PVA and PVA-liposome (PVA-L) formulations. <em>In vitro</em> assays demonstrated the compatibility of meshes with cell growth, ERAP2 engagement and antigen presentation. The results of the study validated the potential for future applications in the specified therapeutic areas.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"690 ","pages":"Article 126555"},"PeriodicalIF":5.2,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145900378","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-02-10Epub Date: 2025-12-20DOI: 10.1016/j.ijpharm.2025.126518
Anika Lins , Marco Fortmann , Dennis Mulac-Hahnen , Hans-Ulrich Humpf , Klaus Langer
This study demonstrates that both the presence and the type of the protein corona have a high impact on the interactions of nanoparticles with cells of the mononuclear phagocyte system. Nanoparticles with an opsonin-rich protein corona are rapidly recognized and taken up by these cells. This results in the clearance of nanoparticles from the bloodstream and their accumulation in liver and spleen. To gain deeper insights into this phenomenon, the protein corona was analyzed using mass spectrometry. Furthermore, nanoparticle interactions with THP-1 monocytes and macrophage-like cells derived from THP-1 monocytes were investigated using fluorescence microscopy and flow cytometry. Specifically, we examined the following aspects: (I) the duration of nanoparticle incubation with immune cells, (II) the type of the protein corona formed, (III) the type of immune cells used, and (IV) the medium used for nanoparticle incubation. We demonstrated that the composition of the hard protein corona, and especially the strength of the enrichment of opsonins, is a key determinant of nanoparticle interaction with immune cells, highlighting the importance of protein corona analysis.
{"title":"The nanoparticle protein corona impacts interactions with monocytes and macrophages","authors":"Anika Lins , Marco Fortmann , Dennis Mulac-Hahnen , Hans-Ulrich Humpf , Klaus Langer","doi":"10.1016/j.ijpharm.2025.126518","DOIUrl":"10.1016/j.ijpharm.2025.126518","url":null,"abstract":"<div><div>This study demonstrates that both the presence and the type of the protein corona have a high impact on the interactions of nanoparticles with cells of the mononuclear phagocyte system. Nanoparticles with an opsonin-rich protein corona are rapidly recognized and taken up by these cells. This results in the clearance of nanoparticles from the bloodstream and their accumulation in liver and spleen. To gain deeper insights into this phenomenon, the protein corona was analyzed using mass spectrometry. Furthermore, nanoparticle interactions with THP-1 monocytes and macrophage-like cells derived from THP-1 monocytes were investigated using fluorescence microscopy and flow cytometry. Specifically, we examined the following aspects: (I) the duration of nanoparticle incubation with immune cells, (II) the type of the protein corona formed, (III) the type of immune cells used, and (IV) the medium used for nanoparticle incubation. We demonstrated that the composition of the hard protein corona, and especially the strength of the enrichment of opsonins, is a key determinant of nanoparticle interaction with immune cells, highlighting the importance of protein corona analysis.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"690 ","pages":"Article 126518"},"PeriodicalIF":5.2,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145809370","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Oleosomes are natural oil bodies extracted from plant seeds and are becoming promising candidates for topical drug-delivery carriers because of their unique structure, biocompatibility, and sustainable nature. This study primarily focuses on exploring the potential of oleosomes with regard to their structural characteristics, extraction strategies, loading approaches, release mechanisms, and their wide range of applications compared with other carrier systems. Current challenges such as the low loading capacity for hydrophilic drugs, lack of regulatory standardization, and allergenicity are being addressed through evolving approaches including hybrid oleosome-liposome systems, recombinant oleosin engineering, and stimulus-responsive coatings. Marketed products and patents further emphasize the translational applicability of oleosome technology. Altogether, oleosomes represent an emerging, environmentally friendly platform for novel topical and transdermal drug delivery systems. These oleosomes are progressing as a multipurpose and scalable platform with significant potential for food, cosmetic, and pharmaceutical applications. From versatile natural emulsions to precision-targeted drug carriers, forthcoming research is converging toward strategies to advance oleosome technology. One such evolving direction is the synthetic molecular biology application to engineer “designer” oleosomes.
{"title":"Oleosomes as emerging Next-Generation carrier for topical drug delivery","authors":"Sumel Ashique , Biplab Debnath , Shayeri Chatterjee Ganguly , Piyali Khamkat , Priya Manna , Md Sadique Hussain , Mohini Mondal , Tahreen Taj , Hitesh Chopra , Sabina Yasmin , Juberahamad Rajjak Attar , Md Yousuf Ansari","doi":"10.1016/j.ijpharm.2025.126545","DOIUrl":"10.1016/j.ijpharm.2025.126545","url":null,"abstract":"<div><div>Oleosomes are natural oil bodies extracted from plant seeds and are becoming promising candidates for topical drug-delivery carriers because of their unique structure, biocompatibility, and sustainable nature. This study primarily focuses on exploring the potential of oleosomes with regard to their structural characteristics, extraction strategies, loading approaches, release mechanisms, and their wide range of applications compared with other carrier systems. Current challenges such as the low loading capacity for hydrophilic drugs, lack of regulatory standardization, and allergenicity are being addressed through evolving approaches including hybrid oleosome-liposome systems, recombinant oleosin engineering, and stimulus-responsive coatings. Marketed products and patents further emphasize the translational applicability of oleosome technology. Altogether, oleosomes represent an emerging, environmentally friendly platform for novel topical and transdermal drug delivery systems. These oleosomes are progressing as a multipurpose and scalable platform with significant potential for food, cosmetic, and pharmaceutical applications. From versatile natural emulsions to precision-targeted drug carriers, forthcoming research is converging toward strategies to advance oleosome technology. One such evolving direction is the synthetic molecular biology application to engineer “designer” oleosomes.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"690 ","pages":"Article 126545"},"PeriodicalIF":5.2,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145906031","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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